Chargement en cours...

Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds

[Image: see text] The design of proteolysis-targeting chimeras (PROTACs) is a powerful small-molecule approach for inducing protein degradation. PROTACs conjugate a target warhead to an E3 ubiquitin ligase ligand via a linker. Here we examined the impact of derivatizing two different BET bromodomain...

Description complète

Enregistré dans:
Détails bibliographiques
Publié dans:J Med Chem
Auteurs principaux: Chan, Kwok-Ho, Zengerle, Michael, Testa, Andrea, Ciulli, Alessio
Format: Artigo
Langue:Inglês
Publié: American Chemical Society 2017
Accès en ligne:https://ncbi.nlm.nih.gov/pmc/articles/PMC5788402/
https://ncbi.nlm.nih.gov/pubmed/28595007
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.6b01912
Tags: Ajouter un tag
Pas de tags, Soyez le premier à ajouter un tag!